CA2623770C - Inhibiteurs pyridopyrimidinoniques de pi3k.alpha. - Google Patents
Inhibiteurs pyridopyrimidinoniques de pi3k.alpha. Download PDFInfo
- Publication number
- CA2623770C CA2623770C CA2623770A CA2623770A CA2623770C CA 2623770 C CA2623770 C CA 2623770C CA 2623770 A CA2623770 A CA 2623770A CA 2623770 A CA2623770 A CA 2623770A CA 2623770 C CA2623770 C CA 2623770C
- Authority
- CA
- Canada
- Prior art keywords
- pyrimidin
- methyl
- ethyl
- compound
- optionally substituted
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Dispersion Chemistry (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La présente invention porte sur des Composés de Formule (I) ainsi que sur les sels ou les solvates de qualité pharmaceutique desdits composés, de même que sur les méthodes de synthèse et d'utilisation desdits composés.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US72457105P | 2005-10-07 | 2005-10-07 | |
| US60/724,571 | 2005-10-07 | ||
| US74371906P | 2006-03-23 | 2006-03-23 | |
| US60/743,719 | 2006-03-23 | ||
| PCT/US2006/039734 WO2007044813A1 (fr) | 2005-10-07 | 2006-10-09 | INHIBITEURS DE PI3Kα DE TYPE PYRIDOPYRIMIDINONE |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2623770A1 CA2623770A1 (fr) | 2007-04-19 |
| CA2623770C true CA2623770C (fr) | 2014-05-27 |
Family
ID=45957942
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2623770A Active CA2623770C (fr) | 2005-10-07 | 2006-10-09 | Inhibiteurs pyridopyrimidinoniques de pi3k.alpha. |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US8044062B2 (fr) |
| EP (2) | EP2322523B1 (fr) |
| JP (1) | JP5461012B2 (fr) |
| KR (3) | KR20140105621A (fr) |
| CN (1) | CN101395155A (fr) |
| AU (1) | AU2006302078B2 (fr) |
| BR (1) | BRPI0617159B8 (fr) |
| CA (1) | CA2623770C (fr) |
| DK (1) | DK1940839T3 (fr) |
| EA (1) | EA016945B1 (fr) |
| ES (1) | ES2432046T3 (fr) |
| GE (1) | GEP20115304B (fr) |
| HR (1) | HRP20130902T1 (fr) |
| IL (1) | IL190292A (fr) |
| NO (1) | NO343136B1 (fr) |
| NZ (2) | NZ594628A (fr) |
| PL (1) | PL1940839T3 (fr) |
| RS (1) | RS52953B (fr) |
| WO (1) | WO2007044813A1 (fr) |
Families Citing this family (58)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100525768C (zh) | 2000-10-23 | 2009-08-12 | 史密丝克莱恩比彻姆公司 | 新化合物 |
| MY145343A (en) * | 2005-03-25 | 2012-01-31 | Glaxo Group Ltd | Novel compounds |
| EA016945B1 (ru) * | 2005-10-07 | 2012-08-30 | Экселиксис, Инк. | ПИРИДОПИРИМИДИНОНОВЫЕ ИНГИБИТОРЫ PI3Kα |
| US7989622B2 (en) * | 2005-10-07 | 2011-08-02 | Exelixis, Inc. | Phosphatidylinositol 3-kinase inhibitors and methods of their use |
| CN102746298A (zh) * | 2005-10-07 | 2012-10-24 | 埃克塞里艾克西斯公司 | PI3Kα的吡啶并嘧啶酮抑制剂 |
| GB0614471D0 (en) | 2006-07-20 | 2006-08-30 | Syngenta Ltd | Herbicidal Compounds |
| CN101528231A (zh) * | 2006-08-16 | 2009-09-09 | 埃克塞利希斯股份有限公司 | 在癌症的治疗中使用pi3k和mek调控剂 |
| PT2074122E (pt) | 2006-09-15 | 2011-08-24 | Pfizer Prod Inc | Compostos de pirido(2,3-d)-pirimidinona e sua utilização como inibidores de pi3 |
| MY150697A (en) * | 2007-04-10 | 2014-02-28 | Exelixis Inc | Methods of treating cancer using pyridopyrimdinone inhibitors of p13k alpha |
| WO2008127594A2 (fr) * | 2007-04-11 | 2008-10-23 | Exelixis, Inc. | Procédés de traitement impliquant l'inhibition de pi3k-alpha au moyen d'inhibiteurs de type quinaxoline |
| CN101711249A (zh) * | 2007-04-11 | 2010-05-19 | 埃克塞里艾克西斯公司 | 作为PI3K-α的抑制剂用于治疗癌症的吡啶并[2,3-D]嘧啶-7-酮化合物 |
| CA2683784A1 (fr) * | 2007-04-11 | 2008-10-23 | Exelixis, Inc. | Composes pyrido [2, 3-d] pyrimidin-7-one utilises en tant qu'inhibiteurs de pi3k-alpha pour le traitement du cancer |
| AR073524A1 (es) * | 2008-09-30 | 2010-11-10 | Exelixis Inc | Piridopirimidinonas inhibidores de pi3k a y m tor |
| TWI378933B (en) | 2008-10-14 | 2012-12-11 | Daiichi Sankyo Co Ltd | Morpholinopurine derivatives |
| JP2010111702A (ja) * | 2009-02-16 | 2010-05-20 | Tetsuya Nishio | 複素環化合物、その製造法および用途 |
| US8591943B2 (en) | 2009-04-09 | 2013-11-26 | Merck Sharp & Dohme Corp. | Pyrazolo[1,5-a]pyrimidine derivatives as mTOR inhibitors |
| WO2011049625A1 (fr) | 2009-10-20 | 2011-04-28 | Mansour Samadpour | Procédé de criblage d'aflatoxine dans des produits |
| NZ599830A (en) | 2009-11-05 | 2014-08-29 | Rhizen Pharmaceuticals Sa | Novel kinase modulators |
| CA2788678C (fr) | 2010-02-03 | 2019-02-26 | Signal Pharmaceuticals, Llc | Identification d'une mutation lkb1 comme biomarqueur de prediction de sensibilite a des inhibiteurs de kinase tor |
| UY33221A (es) | 2010-02-09 | 2011-09-30 | Univ California | MÉTODOS PARA TRATAR CÁNCER USANDO INHIBIDORES DE PI3K Y mTOR EN COMBINACIÓN CON INHIBIDORES DE AUTOFAGIA |
| ES2525866T3 (es) * | 2010-08-05 | 2014-12-30 | Temple University - Of The Commonwealth System Of Higher Education | 8-alquil-7-oxo-7,8-dihidropirido [2,3-d]pirimidina-6-carbonitrilos sustituidos en 2 y usos de los mismos |
| EP2616442B8 (fr) | 2010-09-14 | 2018-10-17 | Exelixis, Inc. | Inhibiteurs de pi3k-delta et leurs procédés d'utilisation et fabrication |
| WO2012065019A2 (fr) | 2010-11-12 | 2012-05-18 | Exelixis, Inc. | Inhibiteurs pyridopyrimidinone de p13k alpha |
| JP2013544827A (ja) * | 2010-11-24 | 2013-12-19 | エクセリクシス, インク. | PI3K/mTORの阻害剤としてのベンゾオキサゼピン類ならびにそれらの使用法および製造法 |
| WO2013043232A2 (fr) * | 2011-04-08 | 2013-03-28 | Afraxis, Inc. | 8-éthyl-6(aryl)pyrido[2,3-d]pyrimidin-7(8h)-ones utilisables en vue du traitement d'affections touchant le système nerveux, ainsi qu'en vue du traitement du cancer |
| CN103635183A (zh) | 2011-04-29 | 2014-03-12 | 埃克塞利希斯股份有限公司 | 使用pi3k/mtor的吡啶并嘧啶抑制剂来治疗淋巴瘤的方法 |
| PH12013502240B1 (en) | 2011-05-04 | 2018-06-27 | Rhizen Pharmaceuticals Sa | Novel compounds as modulators of protein kinase |
| TW201306842A (zh) * | 2011-06-15 | 2013-02-16 | Exelixis Inc | 使用pi3k/mtor吡啶並嘧啶酮抑制劑及苯達莫司汀及/或利妥昔單抗治療惡性血液疾病之組合療法 |
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| WO2013115884A2 (fr) | 2011-11-15 | 2013-08-08 | Trustees Of Boston University | Inhibiteurs de virus, de type pyridopyrimidinone |
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| WO2014172436A1 (fr) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Polythérapie comprenant un inhibiteur de kinase tor et un composé de quinazolinone substitué en 5 pour le traitement du cancer |
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| CA2908742C (fr) | 2013-04-17 | 2021-06-01 | Signal Pharmaceuticals, Llc | Polytherapie comprenant un inhibiteur de la kinase tor et un analogue de la cytidine pour le traitement du cancer |
| CA2909579A1 (fr) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Therapie combinee comprenant un inhibiteur de la kinase tor et du n-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide pour le traitement d'un cancer |
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2006
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- 2006-10-09 ES ES06825768T patent/ES2432046T3/es active Active
- 2006-10-09 PL PL06825768T patent/PL1940839T3/pl unknown
- 2006-10-09 HR HRP20130902TT patent/HRP20130902T1/hr unknown
- 2006-10-09 US US11/988,848 patent/US8044062B2/en active Active
- 2006-10-09 CA CA2623770A patent/CA2623770C/fr active Active
- 2006-10-09 RS RS20130400A patent/RS52953B/sr unknown
- 2006-10-09 KR KR1020147023011A patent/KR20140105621A/ko not_active Ceased
- 2006-10-09 CN CNA2006800370996A patent/CN101395155A/zh active Pending
- 2006-10-09 GE GEAP200610629A patent/GEP20115304B/en unknown
- 2006-10-09 KR KR1020137026515A patent/KR101492795B1/ko not_active Expired - Fee Related
- 2006-10-09 EP EP11157050.3A patent/EP2322523B1/fr active Active
- 2006-10-09 KR KR1020087008369A patent/KR101538412B1/ko not_active Expired - Fee Related
- 2006-10-09 WO PCT/US2006/039734 patent/WO2007044813A1/fr not_active Ceased
- 2006-10-09 NZ NZ594628A patent/NZ594628A/xx not_active IP Right Cessation
- 2006-10-09 BR BRPI0617159A patent/BRPI0617159B8/pt not_active IP Right Cessation
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- 2006-10-09 DK DK06825768.2T patent/DK1940839T3/da active
- 2006-10-09 JP JP2008534787A patent/JP5461012B2/ja not_active Expired - Fee Related
- 2006-10-09 EP EP06825768.2A patent/EP1940839B1/fr active Active
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